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Self-assembled amphiphilic NIR-II emissive nano-micelles for imaging-guided photothermal therapy of colorectal cancer

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Abstract

Colorectal cancer (CRC) is one of the major causes of cancer-related mortality worldwide. Most near-infrared (NIR) agents used in clinical CRC treatment are at NIR-I (700–900 nm) window, which has limitations on deep tissue, and fluorescent probes in the second NIR (1,000–1,700 nm) allow high-resolution bioimaging with deep tissue penetration. However, existing NIR-II fluorophores used in clinical are still rare. Herein, based on shielding-donor-acceptor-donor-shielding (S-D-A-D-S) scaffold, we developed an organic small-molecule fluorophore IR-BTGP with NIR-II emission for imaging-guided photothermal therapy (PTT) in CRC mice model. Amphiphilic IR-BTGP can be self-assembled into spherical nano-micelles, which presents reliable water solubility and photothermal conversion efficiency (30.2%). In vitro experiments indicate that cancer cells treated with IR-BTGP were significantly killed upon 808 nm light irradiation. Furthermore, in vivo NIR-II fluorescence imaging confirms that IR-BTGP accumulates in the tumor region. Remarkably, a significant tumor inhibition rate (78.5%) was observed in tumor-bearing mice when treated with IR-BTGP plus 808 nm irradiation. Therefore, this work shows that IR-BTGP holds great promise as an NIR-II fluorescence imaging-guided PTT platform for CRC in the future.

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Acknowledgements

This work was supported by the National Natural Science Foundation of China (22374065), the Science and Technology Innovation Program of Hunan Province “Huxiang Young Talents Plan” (2021RC3106), and the Key Research and Development Program of Hunan Province, China (2022SK2053).

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Author notes

  1. These authors contributed equally to this work.

Authors and Affiliations

  1. Institute of Molecular Medicine (IMM), Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, 200240, China

    Axin He, Fangfang Xia, Da Han, Qinglai Yang & Weihong Tan

  2. Center for Molecular Imaging Probe, Hunan Province Key Laboratory of Cancer Cellular and Molecular Pathology, Cancer Research Institute, Hengyang Medical School, University of South China, Hengyang, 421001, China

    Qinglai Yang

  3. The Key Laboratory of Zhejiang Province for Aptamers and Theranostics, Zhejiang Cancer Hospital Hangzhou Institute of Medicine (HIM), Chinese Academy of Sciences, Hangzhou, 310022, China

    Weihong Tan

  4. Molecular Science and Biomedicine Laboratory (MBL), State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, College of Biology, Aptamer Engineering Center of Hunan Province, Hunan University, Changsha, 410082, China

    Weihong Tan

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  1. Axin He
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  2. Fangfang Xia
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  3. Da Han
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Correspondence to Qinglai Yang or Weihong Tan.

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Conflict of interest The authors declare no conflict of interest.

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Supporting information The supporting information is available online at chem.scichina.com and link.springer.com/journal/11426. The supporting materials are published as submitted, without typesetting or editing. The responsibility for scientific accuracy and content remains entirely with the authors.

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He, A., Xia, F., Han, D. et al. Self-assembled amphiphilic NIR-II emissive nano-micelles for imaging-guided photothermal therapy of colorectal cancer. Sci. China Chem. (2024). https://doi.org/10.1007/s11426-023-1920-0

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